Pyrrolnitrin and related pyrroles endowed with antibacterial activities against Mycobacterium tuberculosis.

abstract：:The biological activity for a set of melanocortin-4 receptor (MC4R) agonists containing a piperazine core with an ortho-substituted aryl sulfonamide is described. Compounds from this set had binding and functional activities at MC4R less than 30 nM. The most selective compound in this series was >25,000-fold more pote...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fotsch C,Han N,Arasasingham P,Bo Y,Carmouche M,Chen N,Davis J,Goldberg MH,Hale C,Hsieh FY,Kelly MG,Liu Q,Norman MH,Smith DM,Stec M,Tamayo N,Xi N,Xu S,Bannon AW,Baumgartner JW

更新日期：2005-03-15 00:00:00

abstract：:We have succeeded in the acquisition of DNA aptamers that recognize chitin using in vitro selection. The obtained DNA aptamers have the stem-loop or bulge loop structures with guanine rich loop clusters and the clockwise B-form stems. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fukusaki E,Kato T,Maeda H,Kawazoe N,Ito Y,Okazawa A,Kajiyama S,Kobayashi A

更新日期：2000-03-06 00:00:00

abstract：:We report the discovery of a novel azetidine scaffold for colony stimulating factor-1 receptor (CSF-1R) Type II inhibitors by using a structure-based drug design (SBDD) based on a docking model. The work leads to the representative compound 4a with high CSF-1R inhibitory activity (IC50 = 9.1 nM). The obtained crystal ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ikegashira K,Ikenogami T,Yamasaki T,Hase Y,Yamaguchi T,Inagaki K,Doi S,Adachi T,Koga Y,Hashimoto H

更新日期：2019-01-01 00:00:00

abstract：:Extensive SAR studies and optimization of ADME properties of benzimidazol-2-one derivatives led to the identification of BMS-433771 (3) as an orally active RSV fusion inhibitor. In order to extend the structure-activity relationships for this compound series, substitution of the benzimidazole ring was examined with a ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang XA,Cianci CW,Yu KL,Combrink KD,Thuring JW,Zhang Y,Civiello RL,Kadow KF,Roach J,Li Z,Langley DR,Krystal M,Meanwell NA

更新日期：2007-08-15 00:00:00

abstract：:In an effort to find new antibiotics, a novel series of 14-membered macrolides with imidazo[4,5-b]pyridinyl sulfur contained alkyl side chains has been synthesized based on commercially available clarithromycin. Chemical transformation of hydroxy group at position C-3 afforded range of ketolides and acylides. Compared...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu P,Liu L,Chen XZ,Li Y,Liu J,Jin ZP,Wang GQ,Lei PS

更新日期：2009-08-01 00:00:00

abstract：:A new cytotoxic β-carboline alkaloid, 1-methyl-3-(2-hydroxypropan-2-yl)-2-(5-methoxy-9H-β-carbolin-1-yl)-cyclopentanol (1), was isolated from roots of Galianthe thalictroides, together with the alkaloid 1-(hydroxymethyl)-3-(2-hydroxypropan-2-yl)-2-(5-methoxy-9H-β-carbolin-1-yl)-cyclopentanol (2), the anthraquinones 1-...

journal_title：Bioorganic & medicinal chemistry letters

authors： de Oliveira Figueiredo P,Perdomo RT,Garcez FR,de Fatima Cepa Matos M,de Carvalho JE,Garcez WS

更新日期：2014-03-01 00:00:00

abstract：:The authentic standard PBB3 and its precursor N-desmethyl-PBB3 as well as TBS-protected N-desmethyl-PBB3 precursor for radiolabeling were synthesized from 5-bromo-2-nitropyridine, acrolein diethyl acetal, 6-methoxy-2-methylbenzothiazole, and diethylchlorophosphate with overall chemical yield 1% in six steps, 2% in fiv...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang M,Gao M,Xu Z,Zheng QH

更新日期：2015-10-15 00:00:00

abstract：:Novel arylethynyltriazole acyclonucleosides were synthesized and assessed for their anticancer activity on drug-resistant pancreatic cancer MiaPaCa-2 cells. One lead compound was found to have much more potent apoptosis-related antiproliferative effects than gemcitabine, the current first-line treatment for pancreatic...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang M,Xia Y,Fan Y,Rocchi P,Qu F,Iovanna JL,Peng L

更新日期：2010-10-15 00:00:00

abstract：:The use of cell-membrane translocating sequences for intracellular delivery of peptides can be a powerful approach to validate drug discovery targets in cellular settings. To accomplish this, a protocol has been implemented to couple the antennapedia third helix (residues 43-58) to a potent antagonist of the p53/hdm2 ...

journal_title：Bioorganic & medicinal chemistry letters

authors： García-Echeverría C,Furet P,Chène P

更新日期：2001-08-20 00:00:00

abstract：:A series of pentapeptides, based on hMC4R pentapeptide agonist (Bu-His(6)-DPhe(7)-Arg(8)-Trp(9)-Gly(10)-NH(2)), was prepared in which either DPhe(7) or Trp(9) residue was systematically substituted. A number of interesting DPhe surrogates (D-Thi, D-3-CF(3)Phe, D-2-Nal and D-3,4-diClPhe) as well as Trp surrogates (2-Na...

journal_title：Bioorganic & medicinal chemistry letters

authors： Danho W,Swistok J,Cheung AW,Kurylko G,Franco L,Chu XJ,Chen L,Yagaloff K

更新日期：2003-02-24 00:00:00

abstract：:A facile synthesis of 7-epi-(-)-goniofufurone as well as the first synthesis of (-)-crassalactone C was achieved starting from D-xylose. A comparison of their in vitro antitumour activities with those observed for the corresponding naturally occurring enantiomers was provided. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Popsavin V,Benedeković G,Srećo B,Popsavin M,Francuz J,Kojić V,Bogdanović G

更新日期：2008-10-01 00:00:00

abstract：:A series of 1-(quinoliloxypropyl)-4-aryl-piperazines has been synthesized and the target compounds evaluated for atypical antipsychotic activity in apomorphine induced mesh climbing and stereotypic behaviour in mice. The 8-hydroxyquinoline ether derivative 14 has emerged as an important lead compound showing a potenti...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bali A,Malhotra S,Dhir H,Kumar A,Sharma A

更新日期：2009-06-01 00:00:00

abstract：:A series of 14-deoxy-11,12-didehydroandrographolide analogues were synthesized from naturally occurring andrographolide and their cytotoxicity evaluated against nine cancer cell lines including cholangiocarcinoma. Analogues 5a and 5b exhibited the most potent cytotoxicity with ED50s of 3.37 and 3.08 μM on KKU-M213 cel...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sombut S,Bunthawong R,Sirion U,Kasemsuk T,Piyachaturawat P,Suksen K,Suksamrarn A,Saeeng R

更新日期：2017-12-01 00:00:00

abstract：:S1P receptors (S1PR1-5) are a group of GPCRs activated by a high affinity binding with S1P that have important roles in the regulation of the immune system. A potent S1PR agonist FTY720 is an immunomodulator used to treat multiple sclerosis and several 'second generation' drugs are under clinical development. Subtype-...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hur W,Rosen H,Gray NS

更新日期：2017-01-01 00:00:00

abstract：:A novel series of potent zwitterionic uracil GnRH antagonists were discovered that showed reduced liability for CYP3A4 enzyme inhibition. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Regan CF,Guo Z,Chen Y,Huang CQ,Chen M,Jiang W,Rueter JK,Coon T,Chen C,Saunders J,Brown MS,Betz SF,Struthers RS,Yang C,Wen J,Madan A,Zhu YF

更新日期：2008-08-15 00:00:00

abstract：:High throughput cell-based screening led to the identification of 3-aryloxy lactams as potent androgen receptor (AR) antagonists. Refinement of these leads to improve the ADME profile and remove residual agonism led to the discovery of 12, a potent full antagonist with greater oral bioavailability. Improvements in the...

journal_title：Bioorganic & medicinal chemistry letters

authors： Guo C,Kephart S,Ornelas M,Gonzalez J,Linton A,Pairish M,Nagata A,Greasley S,Elleraas J,Hosea N,Engebretsen J,Fanjul AN

更新日期：2012-01-15 00:00:00

abstract：:Two series (4 and 5) of diarylpyridine derivatives were designed, synthesized, and evaluated for anti-HIV-1 activity. The most promising compound, 5e, inhibited HIV-1 IIIB, NL4-3, and RTMDR1 with low nanomolar EC50 values and selectivity indexes of >10,000. The results of this study indicate that diarylpyridine can be...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tian X,Qin B,Lu H,Lai W,Jiang S,Lee KH,Chen CH,Xie L

更新日期：2009-09-15 00:00:00

abstract：:Practical, asymmetric total syntheses of the title phospholipids from a readily available myo-inositol derivative as well as short chain and cross-linkable aminoether analogues are described. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Falck JR,Krishna UM,Capdevila JH

更新日期：2000-08-07 00:00:00

abstract：:Mo(VI) and Mo(V) salts both react selectively with Hantzsch esters to produce substitute pyridines in good-to-excellent yield (75-99%). The remarkable reactivity and selectivity of MoOCl(4) under reflux of acetonitrile and MoCl(5) in dichloromethane at room temperature encouraged us to propose that molybdenum-containi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Litvić M,Regović M,Smic K,Lovrić M,Filipan-Litvić M

更新日期：2012-06-01 00:00:00

abstract：:New N-(1,2-diphenylethyl)piperazines 6 are disclosed as dual serotonin and noradrenaline reuptake inhibitors (SNRI) which may have potential in treating stress urinary incontinence (SUI). In this Letter, we present new data for SNRI PF-526014 (4) including performance in a canine in vivo model of SUI, cardiovascular a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fray MJ,Fish PV,Allan GA,Bish G,Clarke N,Eccles R,Harrison AC,Le Net JL,Phillips SC,Regan N,Sobry C,Stobie A,Wakenhut F,Westbrook D,Westbrook SL,Whitlock GA

更新日期：2010-06-15 00:00:00

abstract：:Based on the molecular modelling studies, a rational modification of the lead molecule was made to develop highly potent compounds showing anti-cancer activity against human breast cancer cell lines MCF 7, MDA-MB-468 and T-47D. The most potent compounds have Log P and total polar surface area 4.4-5.4 and 59.8 Å, respe...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kaur M,Singh P

更新日期：2019-01-01 00:00:00

abstract：:A two-step reaction cascade is applied to the sequence-specific detection of single-stranded DNA, including analyte-triggered re-activation of apo-aldolase by its cofactor Zn(2+) and catalytic conversion of a chromophore. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Graf N,Kassube S,Krämer R

更新日期：2008-09-01 00:00:00

abstract：:Wheat cell-free expression systems based on wheat germ extract (WGE) enable us to briefly synthesize various types of proteins in vitro merely by exogenously adding their mRNA templates. Moreover, it is possible to produce larger amounts of protein by thoroughly removing the endosperm, which contains many translation ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ogawa A,Kutsuna A,Takamatsu M,Okuzono T

更新日期：2019-08-15 00:00:00

abstract：:Here we report a novel class of peptides-d-diaminopropionic acids (Dap)-for gene delivery. These peptides have attractive properties for gene delivery, and the advantage that they can be easily manipulated in relation to their composition, abiding with tailored-design. We characterized the toxicological and biophysica...

journal_title：Bioorganic & medicinal chemistry letters

authors： Viola JR,Strömberg R,Simonson OE,Andaloussi SE,Smith CI,Murtola M

更新日期：2012-09-01 00:00:00

abstract：:Based on the structure of 4-hydroxy-3-methyl-6-phenylbenzofuran-2-carboxylic acid ethyl ester (1), which exhibits selective cytotoxicity against a tumorigenic cell line, (2,4-dimethoxyphenyl)-(4-hydroxy-3-methyl-6-phenylbenzofuran-2-yl)-methanone (18m) was designed and synthesized as a biologically stable derivative c...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hayakawa I,Shioya R,Agatsuma T,Furukawa H,Naruto S,Sugano Y

更新日期：2004-01-19 00:00:00

abstract：:In the search for plants, containing compounds with α-glucosidase inhibitory activity, we found that a methanolic extract from the leaves and twigs of Archidendron clypearia (Jack.) Nielsen significantly inhibited rat intestinal sucrase in vitro. A phytochemical investigation of the aqueous layer of an A. clypearia ex...

journal_title：Bioorganic & medicinal chemistry letters

authors： Thao NP,Luyen BT,Vinh le B,Lee JY,Kwon YI,Kim YH

更新日期：2016-09-01 00:00:00

abstract：:6-Nitroquipazine has been known as one of the most potent and selective inhibitors of serotonin transporter in vitro and in vivo. Nine derivatives of 6-nitroquipazine were synthesized and tested for their potential abilities to displace [3H]citalopram binding to the rat cortical membranes. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee BS,Chu S,Lee BC,Chi DY,Choe YS,Jeong KJ,Jin C

更新日期：2000-07-17 00:00:00

abstract：:Various 1,3,4-oxadiazole derivatives have been synthesized and their antiproliferative properties have been studied. The in vitro screening was performed against androgen dependent (LNCaP) and androgen independent (PC-3) prostate cancer cell lines. Most of the compounds showed promising activity. Among them, compounds...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mochona B,Qi X,Euynni S,Sikazwi D,Mateeva N,Soliman KF

更新日期：2016-06-15 00:00:00

abstract：:A potential anti-HIV and HCV drug candidate is highly desirable as coinfection has become a worldwide public health challenge. A potent compound based on a tetrabutoxy-calix[4]arene scaffold that possesses dual inhibition for both HIV and HCV is described. Structural activity relationship studies demonstrate the effec...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tsou LK,Dutschman GE,Gullen EA,Telpoukhovskaia M,Cheng YC,Hamilton AD

更新日期：2010-04-01 00:00:00

abstract：:Phosphorodiamidate morpholino oligonucleotides (PMOs) have been extensively applied in antisense strategies for gene regulation because of their high stability in serum and low toxicity. However, chain elongation of PMOs requires long reaction time because few efficient methods have been developed for the formation of...

journal_title：Bioorganic & medicinal chemistry letters

authors： Harakawa T,Tsunoda H,Ohkubo A,Seio K,Sekine M

更新日期：2012-02-01 00:00:00